CN102266345A - Nicarbazin and ethopabate preparation and preparation method thereof - Google Patents
Nicarbazin and ethopabate preparation and preparation method thereof Download PDFInfo
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- CN102266345A CN102266345A CN 201110160377 CN201110160377A CN102266345A CN 102266345 A CN102266345 A CN 102266345A CN 201110160377 CN201110160377 CN 201110160377 CN 201110160377 A CN201110160377 A CN 201110160377A CN 102266345 A CN102266345 A CN 102266345A
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- ethopabate
- nicarbazine
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- pharmaceutically acceptable
- solubilizing agent
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Abstract
The invention discloses a nicarbazin and ethopabate emulsion, which comprises the following components in percentage by weight: 3 to 15 percent of nicarbazin, 0.2 to 1 percent of ethopabate, 54 to 95 percent of pharmaceutically-acceptable solvent and 0.1 to 30 percent of pharmaceutically-acceptable cosolvent or pharmaceutically-acceptable solubilizer. The invention also discloses a preparation method for the nicarbazin and ethopabate preparation. The nicarbazin and ethopabate preparation is high in water solubility and stability and easy to store, the bioavailability of medicines is improved, and the curative effect of the medicines is increased.
Description
Technical field
The present invention relates to a kind of veterinary drug preparation and preparation method thereof, especially a kind of nicarbazine that is used to prevent and treat chicken coccidiosis and ethopabate preparation and preparation method thereof.
Background technology
Eimeria is the parasite that causes the coccidiosis of serious harm poultry farming.Nicarbazine all has good prevention effect to the multiple Eimeria of chicken as Eimeria tenella, fragile Eimeria, murder by poisoning Eimeria, Eimeria maxima, heap type Eimeria, Bu Shi Eimeria.Ethopabate has potentiation to the nicarbazine coccidiostat activity.
At present, the common dosage form of nicarbazine, ethopabate mainly contains pre-mixing agent, nano suspension.Because nicarbazine, the shortcoming that the ethopabate pre-mixing agent is poorly soluble in water, administration is inconvenient make its use and curative effect in the animal oral administration be subjected to very big influence.Though disclosed nicarbazine of patent CN101450038A and ethopabate nano suspension have solved the problem of drinking-water administration, but nicarbazine, ethopabate still exist with the form of solid particle, be unfavorable for that nicarbazine, ethopabate absorb, and production process complexity, need equipment such as high pressure homogenization machine, increased cost.
Summary of the invention
For overcoming above-mentioned the deficiencies in the prior art, the invention provides a kind of nicarbazine and ethopabate preparation, this preparation has solved the problem of nicarbazine and ethopabate poorly water-soluble, has increased the curative effect of medicine, has improved bioavailability of medicament.The present invention also provides the preparation method of this nicarbazine and ethopabate preparation, and this method is simple.
The technology used in the present invention is: a kind of nicarbazine and ethopabate preparation, and according to weight percent meter, described preparation comprises following component:
Nicarbazine 3%～15%,
Ethopabate 0.2%～1%,
Acceptable solvent 54%～95%,
Pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent 0.1%～30%;
Wherein, described acceptable solvent is selected from ethyl acetate, Polyethylene Glycol, liquid paraffin, isopropyl myristate, acetic acid, dimethyl sulfoxide, N, one or more in dinethylformamide, decanoyl/octanoyl glycerides, the ethyl oleate;
Described pharmaceutically acceptable cosolvent is selected from ethanolamine, diethanolamine, triethanolamine, nicotiamide, Pyrazinamide, acetamide, urethane, citric acid, sodium citrate, salicylic acid, sodium salicylate, sodium lactate, 5-chloro-salicylic acid, benzyl benzoate, benzoic acid, sodium benzoate, the para-amino benzoic acid one or more;
Described pharmaceutically acceptable solubilizing agent is selected from one or more in castor oil polyoxyethylene ether, Tween 80, the sorbester p17.
As preferably, described preparation comprises following components in weight percentage:
Nicarbazine 3%～15%,
Ethopabate 0.2%～1%,
Acceptable solvent 65%～90%,
Pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent 5%～30%.
More preferably, the weight percentage of described nicarbazine is 3%～13%.More preferably, the weight percentage of described ethopabate is 0.2%～0.8%.More preferably, the content of described pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent is 8%～25%.
Preferably, described acceptable solvent is selected from ethyl acetate, acetic acid, dimethyl sulfoxide, N, one or more in dinethylformamide, the decanoyl/octanoyl glycerides.
Preferably, described pharmaceutically acceptable cosolvent is selected from one or more in sodium lactate, urethane, nicotiamide, para-amino benzoic acid, sodium salicylate, ethanolamine, sodium benzoate, the citric acid.
Nicarbazine of the present invention and ethopabate preparation are prepared by the method that may further comprise the steps:
Described nicarbazine, described ethopabate, described pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent are dissolved in the described acceptable solvent, and constantly stir, until the liquid that forms clear.
Preferably, first with described nicarbazine, described ethopabate, described pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent mix homogeneously before described dissolving step.
The present invention has following beneficial effect:
1, nicarbazine of the present invention and ethopabate preparation have solved the problem of nicarbazine and ethopabate poorly water-soluble first;
2, the present invention uses solubilizing agent or cosolvent, and nicarbazine and ethopabate are dissolved in the solvent, and nicarbazine and ethopabate are existed with the form of solution, has improved bioavailability of medicament, has improved curative effect; Good stability, but filtration sterilization are easy to store;
3, nicarbazine of the present invention and ethopabate preparation have characteristics easy to use, are applicable to the administration of large-scale farming drinking-water, have reduced the personnel's that culture workload greatly;
4, the present invention has the medication of the raising uniformity, prevents inhomogeneous poisoning of part animal or the insufficient problem of part animal-use drug of causing of administration;
5, drug level height of the present invention, using dosage is little, and the distilled water that can further add arbitrary proportion dilutes, and makes things convenient for clinical administration;
6, preparation method of the present invention also has characteristics simple, that be suitable for large-scale industrial production.
The specific embodiment
Following specific embodiment and application examples have been described in detail the present invention, can further be well understood to the present invention by these embodiment and application examples.But they are not limitation of the invention.
Embodiment 1
Take by weighing 12.5g nicarbazine, 0.8g ethopabate, 67.7g N respectively, dinethylformamide, 5g Tween 80,5g sorbester p17,9g citric acid, standby;
At room temperature, with nicarbazine, ethopabate, citric acid, Tween 80, sorbester p17 mix homogeneously, add N, in the dinethylformamide, constantly stir, the liquid until forming clear promptly makes nicarbazine and ethopabate preparation.
Embodiment 2
Take by weighing 6.2g nicarbazine, 0.4g ethopabate, 63.4g acetic acid, 5g decanoyl/octanoyl glycerides, 25.0g castor oil polyoxyethylene ether (EL-40) respectively, standby;
At room temperature, with nicarbazine, ethopabate, decanoyl/octanoyl glycerides, castor oil polyoxyethylene ether (EL-40) mix homogeneously, be dissolved in the acetic acid, and constantly stir, liquid until forming clear promptly makes nicarbazine and ethopabate preparation.
Embodiment 3
Take by weighing 3.1g nicarbazine, 0.2g ethopabate, 73.7g ethyl acetate, 3.0g sodium benzoate, 20g Tween 80 respectively, standby;
At room temperature, will add in the ethyl acetate behind nicarbazine, ethopabate, sodium benzoate, the Tween 80 mix homogeneously, and constantly stir, the liquid until forming clear promptly makes nicarbazine and ethopabate preparation.
Embodiment 4
Take by weighing the 6.2g nicarbazine respectively, the 0.4g ethopabate, 81.4g dimethyl sulfoxide, 7.0g sodium salicylate, 5g ethanolamine, standby;
At room temperature, will add in the dimethyl sulfoxide behind nicarbazine, ethopabate, sodium salicylate, the ethanolamine mix homogeneously, and constantly stir, the liquid until forming clear promptly makes nicarbazine and ethopabate preparation.
Embodiment 5
Take by weighing the 3.1g nicarbazine respectively, the 0.2g ethopabate, 88.7g ethyl acetate, 5.0g nicotiamide, 3g para-amino benzoic acid, standby;
At room temperature, will add in the ethyl acetate behind nicarbazine, ethopabate, nicotiamide, the para-amino benzoic acid mix homogeneously, and constantly stir, the liquid until forming clear promptly makes nicarbazine and ethopabate preparation.
Embodiment 6
Take by weighing the 6.2g nicarbazine respectively, the 0.4g ethopabate, 85.4g dimethyl sulfoxide, 3.0g sodium lactate, 5g urethane, standby;
At room temperature, with nicarbazine, ethopabate, sodium lactate, urethane mix homogeneously, add in the dimethyl sulfoxide and dissolve, and constantly stir, the liquid until forming clear promptly makes nicarbazine and ethopabate preparation.
Embodiment 7
The curative effect contrast test
The chicken group that nicarbazine that nicarbazine that embodiment 1, embodiment 2, embodiment 3, embodiment 4, embodiment 5, embodiment 6 are made and ethopabate preparation (following difference correspondingly is called for short test group 1,2,3,4,5,6) and market are buied and ethopabate pre-mixing agent (hereinafter to be referred as matched group) are applied to suffer from coccidiosis, relatively therapeutic effect:
Matched group: pre-mixing agent 500g is sneaked in the 1000kg feedstuff, and the chicken that suffers from coccidiosis for 20 ages in days searches for food logotype 5 days;
Test group 1: nicarbazine and ethopabate preparation that 500ml embodiment 1 is made add mixing in the 500L water, and the chicken that suffers from coccidiosis for 20 ages in days drinks water logotype 5 days;
Test group 2: nicarbazine and ethopabate preparation that 1000ml embodiment 2 is made add mixing in the 500L water, and the chicken that suffers from coccidiosis for 20 ages in days drinks water logotype 5 days;
Test group 3: nicarbazine and ethopabate preparation that 2000ml embodiment 3 is made add mixing in the 500L water, and the chicken that suffers from coccidiosis for 20 ages in days drinks water logotype 5 days;
Test group 4: nicarbazine and ethopabate preparation that 1000ml embodiment 4 is made add mixing in the 500L water, and the chicken that suffers from coccidiosis for 20 ages in days drinks water logotype 5 days;
Test group 5: nicarbazine and ethopabate preparation that 2000ml embodiment 5 is made add mixing in the 500L water, and the chicken that suffers from coccidiosis for 20 ages in days drinks water logotype 5 days;
Test group 6: nicarbazine and ethopabate preparation that 1000ml embodiment 6 is made add mixing in the 500L water, and the chicken that suffers from coccidiosis for 20 ages in days drinks water logotype 5 days.
Result of the test sees the following form:
| ? | 3 days cure rates | 3 days effective percentage | 5 days cure rates | 5 days effective percentage |
| Matched group | 66% | 71% | 74% | 79% |
| Test group 1 | 89% | 94% | 95% | 98% |
| Test group 2 | 85% | 92% | 94% | 97% |
| Test group 3 | 88% | 96% | 92% | 95% |
| Test group 4 | 80% | 91% | 93% | 95% |
| Test group 5 | 78% | 90% | 88% | 92% |
| Test group 6 | 82% | 93% | 87% | 96% |
The result shows: compare with pre-mixing agent, nicarbazine of the present invention and ethopabate preparation for treating effect obviously are better than pre-mixing agent, and easy to use.
Above content is in conjunction with specific embodiments to further describing that the present invention did, and can not assert that concrete enforcement of the present invention is confined to these explanations.For the general technical staff of the technical field of the invention, without departing from the inventive concept of the premise, can also make some simple deduction or replace, all should be considered as belonging to protection scope of the present invention.
Claims (6)
1. nicarbazine and ethopabate preparation, it is characterized in that: according to weight percent meter, described preparation comprises following component:
Nicarbazine 3%～15%,
Ethopabate 0.2%～1%,
Acceptable solvent 54%～95% and
Pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent 0.1%～30%;
Wherein, described acceptable solvent is selected from ethyl acetate, Polyethylene Glycol, liquid paraffin, isopropyl myristate, acetic acid, dimethyl sulfoxide, N, one or more in dinethylformamide, decanoyl/octanoyl glycerides, the ethyl oleate;
Described pharmaceutically acceptable cosolvent is selected from ethanolamine, diethanolamine, triethanolamine, nicotiamide, Pyrazinamide, acetamide, urethane, citric acid, sodium citrate, salicylic acid, sodium salicylate, sodium lactate, 5-chloro-salicylic acid, benzyl benzoate, benzoic acid, sodium benzoate, the para-amino benzoic acid one or more;
Described pharmaceutically acceptable solubilizing agent is selected from one or more in castor oil polyoxyethylene ether, Tween 80, the sorbester p17.
2. nicarbazine according to claim 1 and ethopabate preparation is characterized in that: according to weight percent meter, described preparation comprises following component:
Nicarbazine 3%～15%,
Ethopabate 0.2%～1%,
Acceptable solvent 65%～90% and
Pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent 5%～30%.
3. nicarbazine according to claim 1 and 2 and ethopabate preparation is characterized in that: described preparation is prepared by the method that may further comprise the steps:
Described nicarbazine, described ethopabate, described pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent are dissolved in the described acceptable solvent, and constantly stir, until the liquid that forms clear.
4. nicarbazine according to claim 3 and ethopabate preparation is characterized in that: elder generation is with described nicarbazine, described ethopabate, described pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent mix homogeneously before described dissolving step.
5. the preparation method of nicarbazine and ethopabate preparation, it is characterized in that: described preparation method may further comprise the steps:
Described nicarbazine, described ethopabate, described pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent are dissolved in the described acceptable solvent, and constantly stir, until the liquid that forms clear.
6. the preparation method of nicarbazine according to claim 5 and ethopabate preparation is characterized in that: elder generation is with described nicarbazine, described ethopabate, described pharmaceutically acceptable cosolvent and/or pharmaceutically acceptable solubilizing agent mix homogeneously before described dissolving step.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110160377 CN102266345B (en) | 2011-06-15 | 2011-06-15 | Nicarbazin and ethopabate preparation and preparation method thereof |
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| CN 201110160377 CN102266345B (en) | 2011-06-15 | 2011-06-15 | Nicarbazin and ethopabate preparation and preparation method thereof |
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| CN102266345A true CN102266345A (en) | 2011-12-07 |
| CN102266345B CN102266345B (en) | 2013-03-13 |
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| CN 201110160377 Expired - Fee Related CN102266345B (en) | 2011-06-15 | 2011-06-15 | Nicarbazin and ethopabate preparation and preparation method thereof |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101450038A (en) * | 2008-12-29 | 2009-06-10 | 天津瑞普生物技术股份有限公司 | Nicarbazin and ethopabate nano suspension agent and preparation method thereof |
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2011
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101450038A (en) * | 2008-12-29 | 2009-06-10 | 天津瑞普生物技术股份有限公司 | Nicarbazin and ethopabate nano suspension agent and preparation method thereof |
Non-Patent Citations (3)
| Title |
|---|
| 《中国优秀硕士学位论文全文数据库》 20061231 刘照云 氟苯尼考溶液剂研制及其稳定性试验和临床疗效研究 中国农业大学 摘要，全文 1-6 , * |
| 《养殖技术顾问》 20110531 王宏军等 兽药的几种主要剂型 224 1-6 , 第5期 * |
| 《北方牧业》 20050530 李京士 等 兽药制剂中增加药物溶解度的常用方法 25 1-6 , * |
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